Synthesis and anti-tumor activity of EF24 analogues as IKKβ inhibitors.
Yao Song
1
,
Weitao Fu
1
,
Ledan Wang
2
,
Jiabing Wang
1
,
Tao Wei
1
,
Peihong Qiu
1
,
Jianzhang Wu
3
,
Wulan Li
4
3
Publication type: Journal Article
Publication date: 2018-01-01
scimago Q1
wos Q1
SJR: 1.142
CiteScore: 11.3
Impact factor: 5.9
ISSN: 02235234, 17683254
PubMed ID:
29351887
Organic Chemistry
Drug Discovery
General Medicine
Pharmacology
Abstract
EF24 is an IKKβ inhibitor (IC50: 72 μM) containing various anti-tumor activities. In this study, a series of EF24 analogs targeting IKKβ were designed and synthesized. Several IKKβ inhibitors with better activities than EF24 were screened out and B3 showed best IKKβ inhibitory (IC50: 6.6 μM). Molecular docking and dynamic simulation experiments further confirmed this inhibitory effect. B3 obviously suppressed the viability of Hela229, A549, SGC-7901 and MGC-803 cells. Then, in SGC-7901 and MGC-803 cells, B3 blocked the NF-κB signal pathway by inhibiting IKKβ phosphorylation, and followed arrested the cell cycle at G2/M phase by suppressing the Cyclin B1 and Cdc2 p34 expression, induced the cell apoptosis by down-regulating Bcl-2 protein and up-regulating cleaved-caspase3. Moreover, B3 significantly reduced tumor growth and suppressed the IKKβ-NF-κB signal pathway in SGC-7901 xenograft model. In total, this study present a potential IKKβ inhibitor as anti-tumor precursor.
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GOST
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Jin R. et al. Synthesis and anti-tumor activity of EF24 analogues as IKKβ inhibitors. // European Journal of Medicinal Chemistry. 2018. Vol. 144. pp. 218-228.
GOST all authors (up to 50)
Copy
Song Y., Fu W., Wang L., Wang J., Wei T., Qiu P., Wu J., Li W. Synthesis and anti-tumor activity of EF24 analogues as IKKβ inhibitors. // European Journal of Medicinal Chemistry. 2018. Vol. 144. pp. 218-228.
Cite this
RIS
Copy
TY - JOUR
DO - 10.1016/j.ejmech.2017.11.077
UR - https://doi.org/10.1016/j.ejmech.2017.11.077
TI - Synthesis and anti-tumor activity of EF24 analogues as IKKβ inhibitors.
T2 - European Journal of Medicinal Chemistry
AU - Song, Yao
AU - Fu, Weitao
AU - Wang, Ledan
AU - Wang, Jiabing
AU - Wei, Tao
AU - Qiu, Peihong
AU - Wu, Jianzhang
AU - Li, Wulan
PY - 2018
DA - 2018/01/01
PB - Elsevier
SP - 218-228
VL - 144
PMID - 29351887
SN - 0223-5234
SN - 1768-3254
ER -
Cite this
BibTex (up to 50 authors)
Copy
@article{2018_Jin,
author = {Yao Song and Weitao Fu and Ledan Wang and Jiabing Wang and Tao Wei and Peihong Qiu and Jianzhang Wu and Wulan Li},
title = {Synthesis and anti-tumor activity of EF24 analogues as IKKβ inhibitors.},
journal = {European Journal of Medicinal Chemistry},
year = {2018},
volume = {144},
publisher = {Elsevier},
month = {jan},
url = {https://doi.org/10.1016/j.ejmech.2017.11.077},
pages = {218--228},
doi = {10.1016/j.ejmech.2017.11.077}
}